Gentian

Scientific Name(s): Gentiana acaulis L., Gentiana lutea L., Gentiana olivieri, Gentiana scabra Bunge.
Common Name(s): Afat, Bitter root, Bitterwort, Felwort, Gall weed, Gentian, Gentiana, Radix Gentianae Lutea

Medically reviewed by Drugs.com. Last updated on Nov 22, 2023.

Clinical Overview

Use

No clinical trials support traditional use of gentian to stimulate appetite, improve digestion, or treat GI complaints. Gentian has also been used as an emmenagogue and to treat wounds, sore throat, arthritic inflammation, and jaundice.

Dosing

Infusions, decoctions, and macerations of gentian roots and rhizomes have been used as a bitter digestive tonic in doses of 1 to 4 g/day. There are no clinical studies to substantiate this dosage recommendation.

Contraindications

Contraindicated in gastric or duodenal ulcer and hypertension.

Pregnancy/Lactation

Documented adverse effects. Avoid use.

Interactions

None well documented.

Adverse Reactions

The extract may cause headache, nausea, and vomiting.

Toxicology

Mutagenicity has been demonstrated for methanolic extracts in Salmonella assays. Acute veratrum alkaloid poisoning has been reported due to accidental contamination of gentian preparations by veratrum.

Scientific Family

• Gentianaceae (gentian)

Botany

Native to the mountains of central and southern Europe, G. lutea is a perennial herb that grows to 1.8 m with erect stems and smooth, oval leaves. The plant produces a cluster of fragrant orange-yellow flowers. The roots and rhizomes are nearly cylindrical, sometimes branched, varying in thickness from 5 to 40 mm. The root and rhizome portions are longitudinally wrinkled. The color of the rhizomes, ranging from dark brown to light tan, appears to be related to the content of bitter principles, because the darker roots have a more persistent, bitter taste. The roots and rhizomes of G. lutea are used medicinally.Meyer 1934, PLANTS 2010, WHO 1999

G. acaulis is a smaller herb with a basal rosette of lance-shaped leaves and generally grows to 10 cm in height. It is native to the European Alps at 914 to 1,524 m above sea level. The entire G. acaulis plant is used medicinally. Numerous species of gentian native to China are used in Chinese traditional medicine. Radix Gentianae Scabrae (known as Chinese or Japanese gentian) is indigenous to Korea, China, and Japan, and contains chemical constituents similar to these of G. lutea.WHO 1999

Related/similar drugs

turmeric, Ginkgo Biloba

History

The gentians have been used for centuries as bitters to stimulate the appetite, improve digestion, and treat a variety of GI complaints (eg, diarrhea, heartburn, stomach ache, vomiting). Stemless gentian usually is consumed as a tea or alcoholic extract, such as Angostura bitters. The extracts are used in a variety of foods, cosmetics, and some antismoking products. The plant has been used externally to treat wounds and internally to treat sore throat, arthritic inflammation, and jaundice. Despite the name, the dye gentian violet is not derived from this plant.DerMarderosian 1988, Leung 1996, WHO 1999

Chemistry

The most characteristic aspect of gentian is its bitter taste imparted by a number of iridoid glycosides, primarily amarogentin, gentiopicrin (about 1.5% in fresh roots), gentiopicroside, and swertiamarin. The speed of drying of the roots affects their properties as medicinal bitters. Slow drying permits enzymatic hydrolysis of gentiopicrin into gentiogenin and glucose, therefore reducing bitterness. Gentian extract is used as a bitter in concentrations of approximately 0.02% in nonalcoholic beverages. The iridoids have been analyzed by thin-layer chromatography, micellar electrokinetic capillary chromatography, and high-performance liquid chromatography mass spectrometry.Bricout 1974, Glatz 2000, Szucs 2002

In addition to iridoids, the roots contain xanthones and triterpenes.Hayashi 1988, Kakuda 2003, Toriumi 2003 The reported pyridine alkaloids gentianine and gentialutine are thought to be artifacts of basic extraction derived from the iridoids. Stemless gentian also contains the xanthone glycoside gentiacauloside. The flowers and leaves of G. lutea contain iridoids, flavonoids, and xanthones.Menkovic 2000

Uses and Pharmacology

Quality clinical trials evaluating the effect of gentian or its chemical constituents are lacking.(WHO 1999)

Analgesic/anti-inflammatory

Animal data

Gentianine and gentiopicroside have been shown to exert a measurable anti-inflammatory and analgesic effect in animals. Extracts of G. lutea were active in carageenan-induced rat paw edema, xylol-induced mouse ear edema, and cotton-pellet granulatoma models. In addition, the extracts were active in several wound-healing models.(Chen 2008, Mathew 2004, Ozturk 2006)

Clinical data

Clinical trials are lacking.

Antimicrobial

Radix Gentianae Lutea and gentian extracts have been shown to exert antibacterial, antifungal, and antiprotozoal effects in vitro.(WHO 1999)

Methanolic extracts of the flowers and leaves of G. lutea demonstrated a wide range of activity against gram-positive and gram-negative bacteria and yeasts. Isolated chemical constituents mangiferin, isogentisin, and gentiopicrin also demonstrated activity.(Savikin 2009, Weckesser 2007) Activity against Helicobacter pylori has been demonstrated in vitro.(Lans 2007, Mahady 2005) Amarogentin and 2 other iridoids inhibited topoisomerase I of Leishmania.(Ray 1996)

Animal data

The roots of G. lutea have been used as an anthelmintic in ethnoveterinary medicine.(Lans 2007)

Clinical data

Clinical trials are lacking.

Hepatic effects

Animal data

In rats, intragastric and intraduodenal administration of gentian extracts stimulated bile production(Liu 2002, WHO 1999) and showed a protective effect on the liver against chemical insults.(Liu 2002)

Clinical data

In an uncontrolled study, stimulation of gall bladder secretions was increased by gentian.(WHO 1999)

GI tract

Bitter substances ingested before meals are reputed to improve the appetite and aid digestion by stimulating the flow of gastric juices and bile. However, because gentian is most often consumed in alcoholic beverages, it is difficult to distinguish the effects of gentian from those of alcohol.

Animal data

Ethanol extracts of the roots and rhizomes of G. lutea have increased gastric secretions in rats and sheep.(WHO 1999)

Clinical data

In 2 uncontrolled clinical studies, stimulation of gastric secretions was increased and GI symptoms (eg, abdominal pain, constipation, dyspepsia, heartburn) were reduced.(WHO 1999)

Other uses

Gentian extracts have hydroxy radical scavenging activity(Calliste 2001, Kusar 2006) and exert a protective effect against ketoconazole-induced testicular damage in rats, assumed to be due to antioxidant effects.(Amin 2008) Gentiopicroside and the essential oil of G. lutea relax smooth muscle in isolated animal trachea and ileum.(Rojas 2000, WHO 1999) Gentian extracts prolong swimming endurance in mice.(Öztürk 2002)

Antidepressant effects were demonstrated in a chronic mild stress model in male rats with G. olivieri ethanolic extract and the positive control both showing significant improvements in appetite, liver indices, antioxidant status, proinflammatory cytokines, as well as levels of serotonin, noradrenaline, and cortisol.(Berk 2020)

G. lutea extract was found to modulate ceramide synthesis in psoriasis-like keratinocytes(Gendrisch 2020) and in healthy volunteers who applied a 5% G. lutea extract cream twice daily for 4 weeks. An increase in lipid production, glucosylceramides, and the expression of enzymes that generate long chain ceramides was observed.(Gendrisch 2020, Wolfle 2017)

Positive effects have been reported for G. lutea on glucose levels in type 1 and 2 diabetic rat models as well as atherosclerotic parameters in other diabetic rat models.(Joskic 2019)

Dosing

The pharmacokinetics and tissue distribution of gentiopicroside after oral and parenteral administration have been studied in mice. It was rapidly absorbed with low bioavailability and rapidly cleared.Wang 2004, Wang 2007

Infusions, decoctions, and macerations of gentian roots and rhizomes have been used as a bitter digestive tonic in doses of 1 to 4 g/day. There are no clinical studies to substantiate this dosage recommendation.WHO 1999

Pregnancy / Lactation

Mutagenic activity has been demonstrated in assays, and G. lutea has been traditionally used as an emmenagogue. Avoid use in pregnancy and lactation.WHO 1999

Interactions

Case reports are lacking; however, hemostatic activity has been demonstrated in vitro for extracts of G. luteaBakuridze 2009 and isogentisin and several other compounds from gentian inhibited monoamine oxidase.Suzuki 1978, Haraguchi 2004 If substantiated in a clinical setting, these properties may have implications for coadministration of anticoagulant or antidepressant medicines.

Adverse Reactions

The extract is usually taken in very small doses that do not appear to cause adverse effects; however, it may cause GI irritation, resulting in nausea and vomiting and, rarely, headache. Radix Gentianae Lutea is contraindicated in GI or duodenal ulcer. Classical texts include hypertension as a contraindication, but the reasons are difficult to substantiate.WHO 1999

Toxicology

Mutagenicity has been demonstrated for methanolic extracts in Salmonella assays.WHO 1999

The highly toxic white hellebore (Veratrum album L.) often grows in close proximity to gentian. Cases of acute veratrum alkaloid poisoning have been reported due to accidental contamination of gentian preparations by veratrum. Identification of esteralkaloids were the suspected cause of resulting nausea, vomiting, oral paraesthesia, hypotension, and severe bradycardia.Garnier 1985, Grobusch 2008, Rauber-Lüthy 2010

Index Terms

• Radix Gentianae Scabrae

References

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